About
Letrozole is a potent and highly selective non-steroidal aromatase inhibitor. It works by competitively binding to the heme of the cytochrome P450 enzyme aromatase, thereby inhibiting the conversion of androgens (like androstenedione and testosterone) into estrogens (estrone and estradiol) in peripheral tissues. In postmenopausal women, estrogen production primarily occurs through this aromatase enzyme, as ovarian function has ceased. By significantly reducing circulating estrogen levels, letrozole deprives hormone-receptor-positive breast cancer cells of the estrogen needed for their growth and proliferation.
This mechanism makes letrozole a highly effective endocrine therapy for breast cancer that is sensitive to estrogen. It is particularly indicated for postmenopausal women, where it has demonstrated superior efficacy compared to tamoxifen in certain settings, reducing the risk of recurrence and improving disease-free survival. Its targeted action on estrogen synthesis minimizes effects on other steroid hormone pathways, making it a valuable agent in hormone-sensitive breast cancer management.
Uses
- Adjuvant treatment of hormone-receptor-positive early breast cancer in postmenopausal women.
- Extended adjuvant treatment of hormone-receptor-positive early breast cancer in postmenopausal women who have completed standard tamoxifen therapy.
- First-line treatment of hormone-receptor-positive advanced breast cancer in postmenopausal women.
- Treatment of advanced breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.
Directions For Use
Take orally once daily, with or without food, as directed by your physician. Swallow the tablet whole.
Benefits
- Highly effective in treating hormone-receptor-positive breast cancer in postmenopausal women.
- Significantly reduces the risk of breast cancer recurrence.
- Improves disease-free survival in adjuvant and extended adjuvant settings.
- Offers a targeted endocrine therapy with a well-established safety profile.
- Can be used as first-line or subsequent therapy for advanced disease.
- Available as an oral tablet for convenient daily administration.
Side Effects
- Hot flashes
- Joint pain (arthralgia)
- Fatigue
- Headache
- Nausea
- Bone pain
- Osteoporosis and fractures
- Hypercholesterolemia (high cholesterol)
- Peripheral edema (swelling)
- Dizziness
- Weight gain
- Vaginal dryness
Safety Measures
- Alcohol - No specific interaction, but excessive alcohol intake can increase the risk of certain cancers and may worsen some side effects like fatigue.
- Pregnancy - Contraindicated in pregnancy due to potential for severe fetal harm. Not for use in premenopausal women unless effective contraception is used.
- Breastfeeding - Not recommended during breastfeeding as it is unknown if letrozole is excreted in human milk and could harm the infant.
- Liver - Use with caution in patients with severe hepatic impairment; dose adjustment may be necessary. Monitor liver function tests.
- Kidney - No dose adjustment is generally required for mild to moderate renal impairment. Use with caution in severe impairment.
- Lung - No specific lung-related safety concerns. However, monitor for any unusual respiratory symptoms in patients with pre-existing conditions.
Disclaimer
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Always consult your doctor for any medical concerns, and discuss your questions about health conditions or medications with a qualified healthcare professional. Do not ignore or delay seeking professional medical advice based on information found on Med E Hub.
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